TAK-683-acetate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETAK-683acetateCat.No.:HY-P2161B分⼦式:C₆₆H₈₇N₁₇O₁₅分⼦量:1358.5SequenceShortening:N-Acetyl-YWNTF{aza}L{Met-R}W-NH2作⽤靶点:Others作⽤通路:Others储存⽅式:Protectfromlight,storedundernitrogenPowder-80°C2years-20°C1yearInsolvent-80°C6months-20°C1monthBIOLOGICALACTIVITY⽣物活性TAK-683acetate⼀种有效的完全KISS1R激动剂(IC50=170pM)，具有改的代谢稳定性。TAK-683acetate⼀个九肽metastin的类似物，针对⼈与⼤⿏EC50值分别为0.96nM和1.6nM。TAK-683acetate消耗下丘脑GnRH，降低⾎浆FSH、LH、酮⽔平，具有研究激素依赖性前列腺癌的潜⼒。体外研究TAK-683acetateexhibitsanIC50value(95%CI)fromreceptorbindingassaysis150-180pMandEC50value(95%CI)fromCa+mobilizationassaysis180(159–203)pMinratKISS1R-expressingChinesehamsterovary(CHO)cells[4].体内研究TAK-683acetate(subcutaneousinjection;0.008,0.08,0.8,or8μmol/ml/kg;oncedaily;7days)inducesanincreaseinplasmaluteinizinghormoneandtestosteronelevels;however,afterday7,plasmahormonelevelsandgenitalorganweightsarereduced[3].TAK-683acetate(subcutaneousinjection;10,30,or100pmol/h;oncedaily;4weeks)providesapromisingforsuppressingreproductivefunctionsandhormone-relateddiseasessuchasprostatecancer[3].TAK-683acetate(subcutaneousinjection;2.1-21nmol/kg/day;oncedaily;12weeks)hasalonger-termevaluationinprostatecancermodel,serumconcentrationsofPSAisreducedinrats,PSAconcentrationsarereducedtobelowthelimitofdetection(0.5ng/ml))inallratsbyday14[4].AnimalModel:MaleSDratwithprostatecancermodel[4]1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEDosage:2.1,7,14,21nmol/kg/dayAdministration:SubcutaneousinjectionResult:Exhibitedasustainedtestosteronesuppressioninrat.REFERENCES[1].NishizawaN,etal.DesignandSynthesisofanInvestigationalNonapeptideKISS1Receptor(KISS1R)Agonist,Ac-d-Tyr-Hydroxyproline(Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH2(TAK-448),withHighlyPotentTestosterone-SuppressiveActivityandExcellentWaterSolubility.JMedChem.2016Oct13;59(19):8804-8811.Epub2016Sep21.[2].AsamiT,etal.Design,synthesis,andbiologicalevaluationofnovelinvestigationalnonapeptideKISS1Ragonistswithtestosterone-suppressiveactivity.JMedChem.2013Nov14;56(21):8298-307.[3].HisanoriMATSUI,etal.FunctionalAnalysesofKisspeptininControllingGonadalFunctionsMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forres